Acarbose

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Glucobay; Belgium: Glucobay; Bulgaria: Glucobay; Cyprus: Glucobay; Czech Republic: Akarboza, Glucobay; Denmark: Glucobay; Finland: Glucobay; France: Glucor; Germany: Acarbose, Glucobay, Karbose; Greece: Glucobay; Hungary: Acarbose, Glucobay; Ireland: Glucobay; Italy: Glicobase, Glucobay; Luxembourg: Glucobay; Malta: Glucobay; Netherlands: Glucobay; Poland: Glucobay; Portugal: Acarbose, Glucobay; Romania: Glucobay; Slovakia: Glucobay; Slovenia: Glucobay; Spain: Acarbosa, Glucobay, Glumida; Sweden: Glucobay; UK: Glucobay.

North America

Canada: Glucobay; USA: Acarbose, Precose.

Latin America

Argentina: Glucobay; Brazil: Aglucose, Glucobay; Mexico: Acarbosa, Glemisal, Glucobay, Incardel, Sincrosa.

Asia

Japan: Glucobay.

Drug combinations

Chemistry

Acarbose: C~25~H~43~NO~18~. Mw: 645.60. (1) D-Glucose, O-4,6-dideoxy-4-[[[1S-(1α,4α,5β,6 α)]-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-(1→4)-; (2) O-4,6-Dideoxy-4-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-(1→4)-D-glucose. CAS-56180-94-0 (1983).

Pharmacologic Category

Antidiabetic Agents; α-Glucosidase Inhibitors. (ATC-Code: A10BF01).

Mechanism of action

Competitive inhibitor of pancreatic α-amylase and membrane-bound intestinal α-glucoside hydrolases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose. Dose-dependent reduction in postprandial serum insulin and glucose peaks. Inhibits the metabolism of sucrose to glucose and fructose.

Therapeutic use

Used as an adjunct in lowering blood glucose in type 2 diabetes mellitus (non-insulin-dependent).

Pregnancy and lactiation implications

Not recommended as routine management of gestational diabetes mellitus or type 2 diabetes mellitus during pregnancy. Caution during lactation.

Unlabeled use

Contraindications

Hypersensitivity to acarbose or any component of the formulation. Patients with the following: diabetic ketoacidosis or cirrhosis, inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, predisposition to intestinal obstruction, chronic intestinal diseases associated with marked disorders of digestion or absorption, deteriorating conditions as a result of increased intestinal gas formation.

Warnings and precautions

Serum transaminase elevations (dose-related). Fulminant hepatitis rarely reported. Advisable to discontinue acarbose and administer insulin if exposure to stress exists (fever, trauma, infection, surgery). Causes a further lowering of blood glucose in combination with a sulfonylurea increasing its hypoglycemic potential. Use not recommended in significant renal impairment and should be used with caution in other patients with renal impairment.

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